Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.
J Nat Prod
; 74(8): 1779-86, 2011 Aug 26.
Article
in En
| MEDLINE
| ID: mdl-21800856
ABSTRACT
The roots of Krameria lappacea are used traditionally against oropharyngeal inflammation. So far, the astringent and antimicrobial properties of its proanthocyanidin constituents are considered to account for the anti-inflammatory effect. The aim of the present study was to characterize pharmacologically a lipophilic extract of K. lappacea roots and several isolated lignan derivatives (1-11) in terms of their putative anti-inflammatory activity. The dichloromethane extract (ID50 77 µg/cm²) as well compounds 1-11 (ID50 0.31-0.60 µmol/cm²) exhibited topical antiedematous properties comparable to those of indomethacin (ID50 0.29 µmol/cm²) in a mouse ear in vivo model. Two of the most potent compounds, 2-(2-hydroxy-4-methoxyphenyl)-5-(3-hydroxypropyl)benzofuran (5) and (+)-conocarpan (7), were studied regarding their time-dependent edema development and leukocyte infiltration up to 48 h after croton oil-induced dermatitis induction, and they showed activity profiles similar to that of hydrocortisone. In vitro studies of the isolated lignan derivatives demonstrated the inhibition of NF-κB, cyclooxygenase-1 and -2, 5-lipoxygenase, and microsomal prostaglandin E2 synthase-1 as well as antioxidant properties, as mechanisms possibly contributing to the observed in vivo effects. The present findings not only support the ethnopharmacological use of K. lappacea roots but also reveal that the isolated lignan derivatives contribute strongly to the anti-inflammatory activity of this herbal drug.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Benzofurans
/
Lignans
/
Krameriaceae
Type of study:
Prognostic_studies
Limits:
Animals
Country/Region as subject:
Europa
Language:
En
Journal:
J Nat Prod
Year:
2011
Document type:
Article
Affiliation country:
Austria